Abstract: The present invention relates to processes for the preparation of eluxadoline. The present invention also provides a compound of Formula V, a process for its preparation, and its use for the preparation of eluxadoline.

Abstract: The present invention provides a cationic lipid, which allow nucleic acids to be easily introduced into cells, represented by formula (I) (wherein: R1 and R2 are, the same or different, alkenyl, etc, and X1 and X3 are hydrogen atoms, or are combined together to form a single bond or alkylene, and X3 is absent or is alkyl, etc, Y is absent or anion, a and b are, the same or different, 0 to 3, and L3 is a single bond, etc, R3 is alkyl, etc, L1 and L2 are —O—, —CO—O— or —O—CO—), a composition comprising the cationic lipid and a nucleic acid, and a method for introducing a nucleic acid into a cell by using the composition comprising the cationic lipid and the nucleic acid, and the like.

Abstract: The present invention relates to novel isocyanate and isothiocyanate compounds, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans and animals. The novel isocyanate and isothiocyanate compounds are distinguished, as compared with the known isocyanate and isothiocyanate compounds, by improved therapeutical breadth, i.e. fewer side effects while having high anti-tumor activity.

Abstract: Activity-generating delivery molecules comprising the structure R3—(C?O)-Xaa-NH—R4 wherein Xaa is any D- or L-amino acid residue with a non-hydrogen, substituted or unsubstituted side chain, R3—(C?O)— and —NH—R4 are independently a long chain group, each long chain group containing one or more carbon-carbon double bonds, and salts, compositions and methods of use thereof. The activity-generating delivery compounds and compositions are useful for generating activity of an active agent in a cell, tissue, or subject.

Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein R1 represents a C1 to C6 alkyl group which may be substituted by one to three groups selected from substituent group A, or the like (substituent group A: a hydroxy group, a halogeno group, a cyano group, a nitro group, an amino group, a carboxy group, a C1 to C3 alkyl group, etc.); R2, R3, and R8 each independently represent a hydrogen atom or a C1 to C3 alkyl group; R4, R5, R6, R7, R9, and R10 each independently represent a hydrogen atom or the like; and R11 represents a hydrogen atom or the like, has TAFIa enzyme inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, or the like.

Abstract: The invention provides an OLED device including an anode, a cathode and a yellow light-emitting layer located therebetween, the light-emitting layer comprising a 9,10-diarylanthracene host; a yellow light-emitting 5,6,11,12-tetraphenyltetracene derivative where as least 1 of the phenyl groups is further substituted and a non-light-emitting diarylamine substituted 9,10-diarylsubstituted anthracene stabuilizer. Devices of the invention provide improvement in features such as stability and efficiency while maintaining excellent color.

Abstract: The present invention relates to a paramagnetic polynuclear metal complex having enhanced self-relaxation rate and thermodynamic stability, and more particularly, to a synthetic method of a novel DTPA-bis-amide-histidine ligand and DTPA-bis-amide-aspartic acid ligand, a novel gadolinium complex ([Gd(L)H2O]) using the ligand, and a paramagnetic polynuclear metal complex using the gadolinium complex. The paramagnetic polynuclear metal complex is able to fix three or more metals (one gadolinium and two metal ions), thereby providing more excellent self-relaxation rate than the commercially available contrast agents. Thus, it can be widely applied to an MRI contrast agent because of meeting the high self-relaxation rate required as a contrast agent of magnetic resonance imaging (MRI).

Abstract: The invention suggests amphoteric lipids wherein one or more amphoteric groups having an isoelectric point between 4 and 9 are substituted on a membranous or membrane-forming amphiphilic substance, as well as liposomes containing such compounds.

Abstract: The present invention relates to novel isocyanate and isothiocyanate compounds, to pharmaceutical compositions comprising them, and to the use thereof in the treatment of cancer diseases in humans and animals. The novel isocyanate and isothiocyanate compounds are distinguished, as compared with the known isocyanate and isothiocyanate compounds, by improved therapeutical breadth, i.e. fewer side effects while having high anti-tumor activity.

Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers, stereoisomers and polymorphs thereof, wherein A, B and R1 are as defined throughout the description and the claims.

Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.

Abstract: The invention relates to the use of open-chain aryl-, heteroaryl- and benzylsulfonamidocarboxylic acids, -carboxylic esters, -carboxamides and -carbonitriles or salts thereof of the formula (I) in which the respective substituents have the meanings given in the description, for increasing stress tolerance in plants with respect to abiotic stress, and also for increasing plant growth and/or for increasing plant yield.

Abstract: Compounds of general formula (I), salts or solvates thereof and pharmaceutical compositions containing same: wherein Z is N or CH or the Z(R1) part is replaced with a covalent bond, m and n is 0, 1, 2 or 3; HET is heteroaryl; X is CF3, halogen, CO-heterocyclyl, COOR3 or CONHR3; R1 is H, (CH2)o-aryl, (CH2)p-heteroaryl, (CH2)q-biphenyl; C(O)—R5; S(O)2—R6; R2 is H, aryl, heteroaryl, Y—(CH2)r-aryl, Y—(CH2)s-heteroaryl, where some of the above substituents may be substituted; Y is O or S; with the exclusion of the compound where HET is 1,3-thiazol, X is COOH, R1 is 4-fluorophenyl and R2 is benzyloxy. The invention also relates to the use of a compound of general formula (I), salts or solvates thereof for the use in the prevention or treatment of diseases where the activation of MMPs is involved in the pathomechanism. In this aspect the use of the above excluded compound is also inventive.

Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.

Abstract: A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, wherein A represents a C3 to C12 cycloalkyl group which may be substituted by one to three selected from a fluoro group, a hydroxy group, a C1 to C6 alkyl group, etc; R1, R2, and R3 each independently represent a hydrogen atom, a fluoro group, or a C1 to C6 alkyl group; R4 represents a hydrogen atom or a prodrug group; and Y represents —CH2—CHR5—CH2—NHR6 (wherein R5 represents a hydrogen atom, a C1 to C6 alkyl group, or a C1 to C6 alkoxy group, and R6 represents a hydrogen atom or a prodrug group), or the like exhibits excellent TAFIa inhibitory activity and is useful as a therapeutic drug for myocardial infarction, angina pectoris, acute coronary syndrome, cerebral infarction, deep vein thrombosis, pulmonary embolism, and the like.

Abstract: The present invention relates to a paramagnetic polynuclear metal complex having enhanced self-relaxation rate and thermodynamic stability, and more particularly, to a synthetic method of a novel DTPA-bis-amide-histidine ligand and DTPA-bis-amide-aspartic acid ligand, a novel gadolinium complex ([Gd(L)H2O]) using the ligand, and a paramagnetic polynuclear metal complex using the gadolinium complex. The paramagnetic polynuclear metal complex is able to fix three or more metals (one gadolinium and two metal ions), thereby providing more excellent self-relaxation rate than the commercially available contrast agents. Thus, it can be widely applied to an MRI contrast agent because of meeting the high self-relaxation rate required as a contrast agent of magnetic resonance imaging (MRI).

Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6 and Z are as defined throughout the description and the claims.

Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and R1, B and Y are as described throughout the description and the claims.

Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.

Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof wherein: A represents and B, R1, R2, R3, R4, R5, R6, R7, Y and Z are as defined throughout the description and the claims.

Abstract: Compounds of general formula (I) below: are characterized in that A represents in particular a C5-C10 heterocyclic group, Y represents in particular a single bond, and B represents in particular an aryl or heteroaryl group.

Abstract: The invention suggests amphoteric lipids wherein one or more amphoteric groups having an isoelectric point between 4 and 9 are substituted on a membranous or membrane-forming amphiphilic substance, as well as liposomes containing such compounds.

Abstract: Disclosed herein are novel benzophenone derivatives represented by formula I, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, a pharmacological composition containing the same, and a use of the composition as therapeutic drugs. The benzophenone derivatives have an inhibition activity of microtubule formation and can be used to treat a normal proliferative state of a malignant tumor by killing the actively proliferating cells.

Abstract: The present invention provides imidazole derivatives of Formula (I) and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of RAGE-mediated diseases such as Alzheimer's Disease. The present invention further relates to methods for the preparation of compounds of Formula (I) and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising such compounds, and the use the such compounds and/or pharmaceutical compositions in treating RAGE-mediated diseases.

Abstract: Nitrogen-containing lipids prepared from the conjugate addition of amines to acrylates, acrylamides, or other carbon-carbon double bonds conjugated to electron-withdrawing groups are described. Methods of preparing these lipids from commercially available starting materials are also provided. These amine-containing lipids or salts forms of these lipids are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these lipids, they are particularly suited for the delivery of polynucleotides. Complexes or nanoparticles containing the inventive lipid and polynucleotide have been prepared. The inventive lipids may also be used to in preparing microparticle for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.

Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.

Abstract: Provided is a compound having a superior acid secretion suppressive action, which shows an antiulcer activity and the like.

Abstract: This invention provides certain compounds, methods of their preparation, pharmaceutical compositions comprising the compounds, and their use in treating human or animal disorders. The compounds of the invention are useful as modulators of the interaction between the receptor for advanced glycated end products (RAGE) and its ligands, such as advanced glycated end products (AGEs), S100/calgranulin/EN-RAGE, ?-amyloid and amphoterin, and for the management, treatment, control, or as an adjunct treatment for diseases in humans caused by RAGE. Such diseases or disease states include acute and chronic inflammation, the development of diabetic late complications such as increased vascular permeability, nephropathy, atherosclerosis, and retinopathy, the development of Alzheimer's disease, erectile dysfunction, and tumor invasion and metastasis.

Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.

Abstract: The present invention is directed to compounds and compositions for the treatment of neurological diseases that cause neurogenic and neuropathic pain, inflammatory diseases, renal ishaemia, cardiovascular disease and other pathologies caused by the presence of endogenous cannabinoids and or other substrates resulting from the metabolic activities of fatty acid amido hydrolase (FAAH). These compounds are represented by the formula alkylene group; a salt thereof, or a hydrate or a solvate of said compound or said salt; where the variables are as defined in the attached specification.

Abstract: The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure (I) wherein R11 is C5-C18 alkyl or C5-C18 alkenyl; Q is selected from the group consisting of C3-C6 optionally substituted cycloalkyl, C3-C6 optionally substituted heterocyclic, C3-C6 optionally substituted aryl C3-C6 optionally substituted heteroaryl and; R2 is selected from the group consisting of H, C1-C4 alkyl, (C1-C4 alkyl)OH and (C1-C4 alkyl)NH2; R23 is H or C1-C4 alkyl, and R15 is a phosphonate ester or a phosphate ester or a pharmaceutically acceptable salt or tautomer thereof.

Abstract: The present invention provides methods, compositions and systems for silylation of substrates, including direct asymmetric silylation of a substrate to provide enantiomerically enriched silylated products.

Abstract: The invention relates to novel compounds and also to methods of treating at least one disease, disorder, or condition associated with amyloidosis using such compounds. Amyloidosis refers to a collection of diseases, disorders, and conditions associated with abnormal deposition of A-beta protein.

Abstract: The invention relates to novel heteroaryl substituted acetone derivatives which inhibit the enzyme phospholipase A2, pharmaceutical preparations containing these compounds and a method of producing these compounds.

Abstract: The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure: structure: wherein R11 is C5-C18 alkyl or C5-C18 alkenyl; Q is C3-C6 optionally substituted cycloalkyl, C3-C6 optionally substituted heterocyclic, C3-C6 optionally substituted aryl C3-C6 optionally substituted heteroaryl or —NH(CO)—; R3 is H, C1-C4 alkyl, (C1-C4 alkyl)OH or (C1-C4 alkyl)NH2; R23 is H or C1-C4 alkyl, and R15 is hydroxy, phosphonate, or wherein X and R12 is O or S; or a pharmaceutically acceptable salt or tautomer thereof.

Abstract: The invention relates to chemical compounds of formula (I): or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.

Abstract: The present invention relates to compounds of formula I: or pharmaceutically acceptable salts or tautomers thereof, which are inhibitors of histone deacetylase (HDAC). The compounds of the present invention are useful for treating cellular proliferative diseases, including cancer. Further, the compounds of the present invention are useful for treating neurodegenerative diseases, schizophrenia and stroke among other diseases.

Abstract: Process for the preparation of 4-(imidazol-1-yl)benzenesulfonamide derivatives of formula I, wherein R1 represents optionally substituted aryl or heteroaryl, which comprises treating a compound of formula II, wherein R1 has the same meaning defined in the formula I and But represents tert-butyl, with an acid. The 4-(imidazol-1-yl)benzenesulfonamide derivatives of formula I are useful as anti-inflammatory agents.

Abstract: Compounds of general formula (I) which are selective beta-3-agonists and useful for the treatment of obesity and type II diabetes. Exemplary compounds are: [4-(1-{3-[2-(3-phenylsulphonylamino-phenyl)-2-hydroxy-ethylamino]-3-methyl-butyl}-1H-imidazol-4-yl)-phenyl]-acetic acid and methyl [4-(1-{3-[2-(3-phenylsulphonylamino-phenyl)-2-hydroxy-ethylamino]-3-methyl-butyl}-1H-imidazol-4-yl)-phenyl]-acetate.

Abstract: Compounds of formula (I), combinations and uses thereof for disease therapy, or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers, stereoisomers and polymorphs thereof, wherein A, B and R? are as defined throughout the description and the claims.

Abstract: N-Substituted (heteroaryl)alkyl sulfilimines are effective at controlling insects.

Abstract: The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R7 have the meanings given in the claims and specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof, the prodrugs thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, processes for preparing these compounds and their use as pharmaceutical compositions.

Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.

Abstract: The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity.

Abstract: Novel compounds, compositions comprising compounds, and methods for methods for preparing and using compounds are described herein. Methods of treating or ameliorating various conditions, including insulin resistance, pancreatic beta cell apoptosis, obesity, pro-thrombotic conditions, myocardial infarction, hypertension, dyslipidemia, manifestations of Syndrome X, congestive heart failure, inflammatory disease of the cardiovascular system, atherosclerosis, sepsis, type 1 diabetes, liver damage, and cachexia, by administering compounds described herein. Compounds presented herein may be used to modulate serine palmitoyl transferase activity.

Abstract: The invention provides Aryl substituted imidazoles, pyrazoles, pyridizines and related compounds of the Formula where the variables are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of the invention act bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptos. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory and immune system disorders.

Abstract: The present invention relates to S1P analogs that have activity as S1P receptor modulating agents and the use of such compounds to treat diseases associated with inappropriate S1P receptor activity. The compounds have the general structure (I), wherein R1 is C8–C22 alkyl, C8–C22 alkenyl or R12 is O, or R1 and R12 taken together form an optionally substituted aryl or an optionally substituted heteroaryl; R17 is H, alkyl or alkylaryl; R18 is N or CH; R2 and R3 are independently selected from the group consisting of H, NH2, and OH, with the proviso that at least one of R2 and R3 is NH2; R4 is selected from the group consisting of hydroxyl, phosphate, phosphonate methylene phosphonate, ?-substituted methylene phosphonate, thiophoasphate and thiophosphonate; and R5 is C8–C22alkenyl.

Abstract: This invention relates to compounds which are alpha-1 receptor agonists, preferably alpha-1A/L receptor agonists, and which are represented by Formula I: wherein m, A, X, Y, R1, R2, R3, R4 and R5 are as defined in the specification; or individual isomers, racemic or non-racemic mixtures of isomers, or pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds, methods for their use as therapeutic agents, and methods of preparation thereof.

Abstract: The present invention provides a method of treating Alzheimer's disease using a compound of Formula (I). Also provided is a method of inhibiting the aggregation of amyloid proteins using a compound of the Formula (I) and a method of imaging amyloid deposits, as well as new compounds of Formula (I).